发明授权
- 专利标题: Imidazole derivatives having affinity for &agr;2 receptors
- 专利标题(中): 对α2受体具有亲和力的咪唑衍生物
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申请号: US09904836申请日: 2001-07-16
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公开(公告)号: US06479530B2公开(公告)日: 2002-11-12
- 发明人: Arto Karjalainen , Paavo Huhtala , Juha-Matti Savola , Siegfried Wurster , Maire Eloranta , Maarit Hillilä , Raimo Saxlund , Victor Cockcroft , Arja Karjalainen
- 申请人: Arto Karjalainen , Paavo Huhtala , Juha-Matti Savola , Siegfried Wurster , Maire Eloranta , Maarit Hillilä , Raimo Saxlund , Victor Cockcroft , Arja Karjalainen
- 优先权: GB9520150 19951003
- 主分类号: A61K314164
- IPC分类号: A61K314164
摘要:
Imidazole derivatives of formula I wherein n is 0 or 1, R1 is hydrogen or C1-C4-alkyl, R2 is hydrogen or R2 and R3 together form a double bond, R3 is hydrogen or C1-C4-alkyl or R2 and R3 together form a double bond, R4 is hydrogen, C1-C4-alkyl, hydroxy or C1-C4-alkoxy, R5 is hydrogen or C1-C4-alkyl or R4 and R5 together with the carbon atom to which they are attached form a carbonyl group, R6, R7 and R8 are each the same or different and are independently hydrogen, C1-C4-alkyl or C2-C4-alkenyl, C3-C7-cycloalkyl, hydroxy, C1-C4-alkoxy, C1-C4-hydroxyalkyl, thiol, C1-4-alkylthio, C1-4-alkylthiol, halogen, trifluoromethyl, nitro or optionally substituted amino, X is —CHR9—(CHR10)m—, m is 0 or 1, and R9 and R10 are each the same or different and are independently hydrogen or C1-C4-alkyl; or a pharmaceutically acceptable ester or salt thereof, their preparation, use and pharmaceutical compositions comprising them are described. The compounds have affinity for alpha2 receptors and are useful e.g. in the treatment of hypertension, glaucoma, chronic or acute pain, migraine, diarrhea, common cold, ischemia, addiction to chemical substances, anxiety, especially preoperative anxiety and different neurological, musculoskeletal, psychiatric and cognition disorders or as adjuncts to anesthesia.
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